New 2-amino-1,3-thiazine and -thiazepine derivs.

摘要

2-Amino-5,6-dihydro-4H-1,3-thiazine and 2-amino-4,5,6,7-tetrahydro-1,3-thiazepine derivs. of formula (I) and their salts are new: R1 = H, cycloalkyl, or opt. substd. alkyl, alkenyl, alkynyl, aryl, heteroaryl or aralkyl; R2-R5 = H or opt. substd. alkyl; or R1+R2 or R1+R3 = (CH2)n; n = 1-6; A = O, S or NH; m, p = 0 or 1; provided that 2-amino-5,6-dihydro-4H-1,3-thiazine and its 4-methyl, 6-methyl, 4-phenyl, 4-p-tolyl and 4-ethoxy derivs. are excluded. Also claimed are (i) pharmaceutical compsns. contg. sufficient (I) to inhibit nitric oxide synthase (NOS) activity, without the above proviso but excluding 2-amino-5,6-dihydro-6-methyl-4H-1,3-thiazine and a carrier, and (b) the use of (I), without the above proviso, for preparing medicaments for treating symptoms of excessive nitric oxide synthesis in vivo. 29 Cpds. (I) are specifically claimed e.g. (R)-2-amino-5,6-dihydro-4-propyl-4H-1,3-thiazine and (S)-2-amino-5,6-dihydro-4-methoxymethyl-4H-1,3-thiazine.